JP7033588B2 - 癌の治療に有用なparp1、parp2、および/またはチューブリンの阻害剤としてのフタラジン誘導体 - Google Patents
癌の治療に有用なparp1、parp2、および/またはチューブリンの阻害剤としてのフタラジン誘導体 Download PDFInfo
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- JP7033588B2 JP7033588B2 JP2019519615A JP2019519615A JP7033588B2 JP 7033588 B2 JP7033588 B2 JP 7033588B2 JP 2019519615 A JP2019519615 A JP 2019519615A JP 2019519615 A JP2019519615 A JP 2019519615A JP 7033588 B2 JP7033588 B2 JP 7033588B2
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- 0 *c(cc1nc(NC(O*)=O)[n]c1c1)c1-c1c[o]c(CC(c2c3cccc2)=NNC3=O)c1 Chemical compound *c(cc1nc(NC(O*)=O)[n]c1c1)c1-c1c[o]c(CC(c2c3cccc2)=NNC3=O)c1 0.000 description 20
- DCSUGHIXMFUMOQ-UHFFFAOYSA-N CCOC(Nc1nc2cc(-c3cc(CC(c4ccccc44)=NNC4=O)ccc3F)ccc2[nH]1)=O Chemical compound CCOC(Nc1nc2cc(-c3cc(CC(c4ccccc44)=NNC4=O)ccc3F)ccc2[nH]1)=O DCSUGHIXMFUMOQ-UHFFFAOYSA-N 0.000 description 1
- KHBXLYPOXVQKJG-UHFFFAOYSA-N COC(N/C(/SC)=N/C(OC)=O)=O Chemical compound COC(N/C(/SC)=N/C(OC)=O)=O KHBXLYPOXVQKJG-UHFFFAOYSA-N 0.000 description 1
- NVIQLRKCRFZLMN-UHFFFAOYSA-N COC(Nc([nH]c1c2)nc1ccc2-c1cc(CC(c2ccccc22)=NNC2=O)ccc1F)=O Chemical compound COC(Nc([nH]c1c2)nc1ccc2-c1cc(CC(c2ccccc22)=NNC2=O)ccc1F)=O NVIQLRKCRFZLMN-UHFFFAOYSA-N 0.000 description 1
- VYNDWLDIOOXDCP-UHFFFAOYSA-N NC(Nc1nc2cc(-c3cc(CC(c4ccccc44)=NNC4=O)ccc3F)ccc2[nH]1)=O Chemical compound NC(Nc1nc2cc(-c3cc(CC(c4ccccc44)=NNC4=O)ccc3F)ccc2[nH]1)=O VYNDWLDIOOXDCP-UHFFFAOYSA-N 0.000 description 1
- HIGLVUSSPUXZQQ-UHFFFAOYSA-N Nc(c(N)c1)ccc1-c1cc(CC(c2ccccc22)=NNC2=O)ccc1F Chemical compound Nc(c(N)c1)ccc1-c1cc(CC(c2ccccc22)=NNC2=O)ccc1F HIGLVUSSPUXZQQ-UHFFFAOYSA-N 0.000 description 1
- VYXPPUARJNTTAT-UHFFFAOYSA-N Nc1nc2cc(-c3cc(CC(c4ccccc44)=NNC4=O)ccc3F)ccc2[nH]1 Chemical compound Nc1nc2cc(-c3cc(CC(c4ccccc44)=NNC4=O)ccc3F)ccc2[nH]1 VYXPPUARJNTTAT-UHFFFAOYSA-N 0.000 description 1
- DEPDDPLQZYCHOH-UHFFFAOYSA-N Nc1ncc[nH]1 Chemical compound Nc1ncc[nH]1 DEPDDPLQZYCHOH-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021192564A JP2022037004A (ja) | 2016-06-24 | 2021-11-26 | 癌の治療に有用なparp1、parp2、および/またはチューブリンの阻害剤としてのフタラジン誘導体 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662354449P | 2016-06-24 | 2016-06-24 | |
| US62/354,449 | 2016-06-24 | ||
| US201662426095P | 2016-11-23 | 2016-11-23 | |
| US62/426,095 | 2016-11-23 | ||
| PCT/US2017/039119 WO2017223516A1 (en) | 2016-06-24 | 2017-06-23 | Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021192564A Division JP2022037004A (ja) | 2016-06-24 | 2021-11-26 | 癌の治療に有用なparp1、parp2、および/またはチューブリンの阻害剤としてのフタラジン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019522681A JP2019522681A (ja) | 2019-08-15 |
| JP2019522681A5 JP2019522681A5 (https=) | 2021-05-20 |
| JP7033588B2 true JP7033588B2 (ja) | 2022-03-10 |
Family
ID=59297390
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019519615A Active JP7033588B2 (ja) | 2016-06-24 | 2017-06-23 | 癌の治療に有用なparp1、parp2、および/またはチューブリンの阻害剤としてのフタラジン誘導体 |
| JP2021192564A Pending JP2022037004A (ja) | 2016-06-24 | 2021-11-26 | 癌の治療に有用なparp1、parp2、および/またはチューブリンの阻害剤としてのフタラジン誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021192564A Pending JP2022037004A (ja) | 2016-06-24 | 2021-11-26 | 癌の治療に有用なparp1、parp2、および/またはチューブリンの阻害剤としてのフタラジン誘導体 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US11072600B2 (https=) |
| EP (1) | EP3475272B1 (https=) |
| JP (2) | JP7033588B2 (https=) |
| KR (1) | KR102494294B1 (https=) |
| CN (1) | CN109843874B (https=) |
| AU (1) | AU2017280334C1 (https=) |
| ES (1) | ES2964531T3 (https=) |
| HU (1) | HUE066216T2 (https=) |
| IL (1) | IL263917B (https=) |
| MX (2) | MX387726B (https=) |
| PL (1) | PL3475272T3 (https=) |
| PT (1) | PT3475272T (https=) |
| SG (1) | SG11201811393WA (https=) |
| WO (1) | WO2017223516A1 (https=) |
| ZA (2) | ZA201808562B (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3298005B1 (en) | 2015-05-21 | 2024-01-24 | The Regents of The University of California | Anti-cancer compounds |
| EP3383852A4 (en) * | 2015-11-30 | 2019-08-28 | Children's Medical Center Corporation | COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISEASES |
| WO2017223516A1 (en) * | 2016-06-24 | 2017-12-28 | The Regents Of The University Of California | Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer |
| WO2019194738A1 (en) * | 2018-04-05 | 2019-10-10 | Noviga Research Ab | Novel combinations of a tubulin polymerization inhibitor and a poly (adp-ribose) polymerase (parp) inhibitor for use in the treatment of cancer |
| CN112574122B (zh) * | 2019-09-27 | 2024-05-31 | 上海天慈国际药业有限公司 | 一种奥拉帕尼关键中间体的制备方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008114023A2 (en) | 2007-03-22 | 2008-09-25 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| JP2016504347A (ja) | 2012-12-31 | 2016-02-12 | カディラ・ヘルスケア・リミテッド | 置換フタラジン‐1(2h)‐オン誘導体 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3401171A (en) | 1966-03-11 | 1968-09-10 | Smithkline Corp | 2-amidobenzimidazoles |
| SU1019810A1 (ru) | 1981-07-28 | 1991-04-07 | Институт медицинской паразитологии и тропической медицины им.Е.И.Марциновского | Метиловый эфир 5(6)-[1-(2Н)-фталазинонил-4]-1Н-бензимидазолил-2-карбаминовой кислоты, обладающий антигельминтной активностью |
| SU1218649A1 (ru) | 1984-09-19 | 1991-04-30 | Институт медицинской паразитологии и тропической медицины им.Е.И.Марциновского | Способ получени метилового эфира 5(6)-[1(2Н)-фталазинонил-4-]-1Н-бензимидазолил-2-карбаминовой кислоты формулы |
| EP1060166A1 (de) | 1998-02-03 | 2000-12-20 | Boehringer Ingelheim Pharma KG | 5-gliedrige benzokondensierte heterocyclen als antithrombotika |
| KR20010101675A (ko) | 1999-01-26 | 2001-11-14 | 우에노 도시오 | 2h-프탈라진-1-온 유도체 및 그 유도체를 유효 성분으로하는 약제 |
| DE19907813A1 (de) | 1999-02-24 | 2000-08-31 | Boehringer Ingelheim Pharma | Substituierte bicyclische Heterocyclen, deren Herstellung und deren Verwendung als Arzneimittel |
| HU228960B1 (hu) | 2000-10-30 | 2013-07-29 | Kudos Pharm Ltd | Ftalazinon-származékok |
| US7151102B2 (en) | 2000-10-30 | 2006-12-19 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| AR042956A1 (es) | 2003-01-31 | 2005-07-13 | Vertex Pharma | Inhibidores de girasa y usos de los mismos |
| PL1633724T3 (pl) | 2003-03-12 | 2011-10-31 | Kudos Pharm Ltd | Pochodne ftalazynonu |
| WO2005112932A2 (en) | 2004-05-07 | 2005-12-01 | Exelixis, Inc. | Raf modulators and methods of use |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| CN101291928A (zh) * | 2005-10-19 | 2008-10-22 | 库多斯药物有限公司 | 4-杂芳甲基取代的酞嗪酮衍生物 |
| UY30639A1 (es) | 2006-10-17 | 2008-05-31 | Kudos Pharm Ltd | Derivados sustituidos de 2h-ftalazin-1-ona, sus formas cristalinas, proceso de preparacion y aplicaciones |
| CN101981013B (zh) * | 2008-03-27 | 2013-05-29 | 詹森药业有限公司 | 作为parp和微管蛋白聚合抑制剂的四氢菲啶酮和四氢环戊二烯并喹啉酮 |
| EP2529235B1 (en) | 2010-01-29 | 2019-03-06 | Metanomics GmbH | Means and methods for diagnosing heart failure in a subject |
| CN102372706A (zh) | 2010-08-09 | 2012-03-14 | 江苏恒瑞医药股份有限公司 | 酞嗪酮类衍生物、其制备方法及其在医药上的应用 |
| TWI577693B (zh) | 2011-05-31 | 2017-04-11 | 江蘇康緣藥業股份有限公司 | 聚(adp-核糖)聚合酶之三環抑制劑 |
| KR101546743B1 (ko) * | 2012-01-16 | 2015-08-24 | 한국과학기술원 | 인돌 유도체 화합물, 이를 포함하는 Abl 키나제 저해제 조성물 및 이상세포 성장 질환의 예방 및 치료용 약학 조성물 |
| TWI527811B (zh) | 2013-05-09 | 2016-04-01 | 吉李德科學股份有限公司 | 作爲溴結構域抑制劑的苯並咪唑衍生物 |
| WO2017223516A1 (en) * | 2016-06-24 | 2017-12-28 | The Regents Of The University Of California | Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer |
-
2017
- 2017-06-23 WO PCT/US2017/039119 patent/WO2017223516A1/en not_active Ceased
- 2017-06-23 EP EP17737132.5A patent/EP3475272B1/en active Active
- 2017-06-23 CN CN201780051422.3A patent/CN109843874B/zh active Active
- 2017-06-23 SG SG11201811393WA patent/SG11201811393WA/en unknown
- 2017-06-23 PT PT177371325T patent/PT3475272T/pt unknown
- 2017-06-23 IL IL263917A patent/IL263917B/en unknown
- 2017-06-23 MX MX2018015893A patent/MX387726B/es unknown
- 2017-06-23 HU HUE17737132A patent/HUE066216T2/hu unknown
- 2017-06-23 PL PL17737132.5T patent/PL3475272T3/pl unknown
- 2017-06-23 JP JP2019519615A patent/JP7033588B2/ja active Active
- 2017-06-23 KR KR1020197002267A patent/KR102494294B1/ko active Active
- 2017-06-23 AU AU2017280334A patent/AU2017280334C1/en active Active
- 2017-06-23 ES ES17737132T patent/ES2964531T3/es active Active
- 2017-06-23 US US16/310,606 patent/US11072600B2/en active Active
-
2018
- 2018-12-17 MX MX2021013641A patent/MX2021013641A/es unknown
- 2018-12-19 ZA ZA2018/08562A patent/ZA201808562B/en unknown
-
2019
- 2019-07-30 US US16/526,620 patent/US10640493B2/en active Active
-
2021
- 2021-07-15 US US17/376,577 patent/US12145925B2/en active Active
- 2021-11-26 JP JP2021192564A patent/JP2022037004A/ja active Pending
-
2023
- 2023-01-25 ZA ZA2023/01066A patent/ZA202301066B/en unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008114023A2 (en) | 2007-03-22 | 2008-09-25 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| JP2016504347A (ja) | 2012-12-31 | 2016-02-12 | カディラ・ヘルスケア・リミテッド | 置換フタラジン‐1(2h)‐オン誘導体 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3475272A1 (en) | 2019-05-01 |
| US12145925B2 (en) | 2024-11-19 |
| CA3029004A1 (en) | 2017-12-28 |
| IL263917B (en) | 2022-07-01 |
| US20190352283A1 (en) | 2019-11-21 |
| ZA201808562B (en) | 2023-12-20 |
| US20190337928A1 (en) | 2019-11-07 |
| CN109843874B (zh) | 2022-05-27 |
| US10640493B2 (en) | 2020-05-05 |
| CN109843874A (zh) | 2019-06-04 |
| AU2017280334A1 (en) | 2019-01-17 |
| MX2018015893A (es) | 2019-08-01 |
| BR112018076821A2 (pt) | 2019-04-02 |
| MX2021013641A (es) | 2022-01-06 |
| KR20190033534A (ko) | 2019-03-29 |
| AU2017280334C1 (en) | 2022-10-20 |
| KR102494294B1 (ko) | 2023-01-31 |
| AU2017280334B2 (en) | 2021-07-29 |
| JP2019522681A (ja) | 2019-08-15 |
| ZA202301066B (en) | 2024-05-30 |
| PL3475272T3 (pl) | 2024-04-29 |
| HUE066216T2 (hu) | 2024-07-28 |
| US11072600B2 (en) | 2021-07-27 |
| PT3475272T (pt) | 2023-12-15 |
| WO2017223516A1 (en) | 2017-12-28 |
| US20220402894A1 (en) | 2022-12-22 |
| ES2964531T3 (es) | 2024-04-08 |
| SG11201811393WA (en) | 2019-01-30 |
| MX387726B (es) | 2025-03-18 |
| IL263917A (en) | 2019-02-28 |
| EP3475272B1 (en) | 2023-09-13 |
| JP2022037004A (ja) | 2022-03-08 |
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